Perilor
Generic Name
Irinotecan
Manufacturer
Intas Pharmaceuticals
Country
India
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Description
Overview of the medicine
Irinotecan (Perilor) is a chemotherapeutic agent used in the treatment of various cancers, primarily metastatic colorectal cancer. It works by inhibiting DNA topoisomerase I, an enzyme critical for DNA replication, leading to cell death in rapidly growing cancer cells.
Uses & Indications
Dosage
Adults
Metastatic Colorectal Cancer: As a single agent, 125 mg/m² IV infusion over 90 minutes weekly for 4 weeks, followed by a 2-week rest period. Or, in combination, typically 180 mg/m² IV every 2 weeks or 350 mg/m² IV every 3 weeks, as part of a multi-drug regimen.
Elderly
No specific dose adjustment based solely on age, but consider overall health, comorbidities, and hepatic/renal function. Increased toxicity may be observed.
Renal_impairment
Use with caution. Data limited. Dose adjustments may be necessary for severe impairment. Not recommended if creatinine clearance < 60 mL/min.
How to Take
Administered by intravenous infusion over 30 to 90 minutes, usually through a central venous catheter. It must be diluted in 5% Dextrose Injection, USP, or 0.9% Sodium Chloride Injection, USP, prior to administration.
Mechanism of Action
Irinotecan and its active metabolite SN-38 act as topoisomerase I inhibitors. They bind to the topoisomerase I-DNA complex, preventing the re-ligation of DNA single-strand breaks and leading to DNA damage and ultimately apoptosis in cancer cells during DNA synthesis.
Pharmacokinetics
Onset
Not applicable for therapeutic onset; pharmacological effect starts with binding to topoisomerase I. Clinical benefits are observed over treatment cycles.
Excretion
Approximately 25-50% of the dose is excreted in the bile and feces, primarily as SN-38 and SN-38G. About 10-20% is excreted in the urine as parent drug and metabolites.
Half life
Parent drug: approximately 6-12 hours. Active metabolite (SN-38): approximately 10-20 hours.
Absorption
Administered intravenously, resulting in 100% bioavailability. Peak plasma concentrations are achieved at the end of the infusion.
Metabolism
Primarily metabolized in the liver. Irinotecan is converted to its active metabolite SN-38 by carboxylesterase enzymes. SN-38 is then glucuronidated by UDP-glucuronosyltransferase 1A1 (UGT1A1) to an inactive form (SN-38G). Irinotecan is also metabolized by CYP3A4.
Side Effects
Contraindications
- •Patients with severe myelosuppression (neutrophil count < 1.5 x 10^9/L or platelet count < 100 x 10^9/L)
- •Patients with chronic inflammatory bowel disease or bowel obstruction
- •Known hypersensitivity to irinotecan or any excipients
- •Severe hepatic impairment (bilirubin > 3 times upper limit of normal)
Drug Interactions
Neuromuscular blocking agents
Irinotecan has anticholinesterase activity, potentially prolonging neuromuscular blockade (e.g., succinylcholine) or antagonizing non-depolarizing agents.
Laxatives, diuretics, anticholinergic agents
Increased risk or exacerbation of diarrhea. Use with caution.
CYP3A4 Inducers (e.g., Phenytoin, Carbamazepine, Rifampin, St. John's Wort)
May decrease exposure to irinotecan and its active metabolite SN-38, potentially reducing efficacy. Avoid co-administration if possible.
CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Indinavir, Atazanavir, Ritonavir, Clarithromycin)
May increase exposure to irinotecan and SN-38, increasing toxicity. Use with caution and consider dose reduction.
Storage
Store intact vials at 20-25°C (68-77°F), excursions permitted to 15-30°C (59-86°F). Protect from light. Do not freeze. Diluted solutions are stable for 24 hours at room temperature or 48 hours under refrigeration (2-8°C).
Overdose
Management of overdose should include supportive measures aimed at preventing dehydration due to diarrhea and treating any infections due to myelosuppression. Atropine may be used for cholinergic symptoms.
Pregnancy & Lactation
Pregnancy Category D: Irinotecan can cause fetal harm when administered to a pregnant woman. Women of childbearing potential should use effective contraception during treatment and for a specified period after. Lactation: It is unknown whether irinotecan or its metabolites are excreted in human milk. Due to potential serious adverse reactions in breastfed infants, breastfeeding is not recommended during treatment.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
Typically 24 to 36 months when stored unopened under recommended conditions. Diluted solutions have a shorter shelf life (e.g., 24 hours at room temperature, 48 hours refrigerated).
Availability
Hospitals, oncology centers
Approval Status
FDA and DGDA approved
Patent Status
Expired, generic versions available
WHO Essential Medicine
YesAlternative Medicines in Bangladesh
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Global Brand Names
International brand names for this medicine
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